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1.
Psychopharmacology (Berl) ; 197(4): 591-600, 2008 May.
Artigo em Inglês | MEDLINE | ID: mdl-18264695

RESUMO

RATIONALE: Tiagabine is an anticonvulsant drug which may also have sleep-enhancing properties. It acts by inhibiting reuptake at the gamma-aminobutyric acid (GABA) transporter (GAT-1). OBJECTIVES: The aim of the study was to determine whether tiagabine acted as a discriminative stimulus and, if so, whether other GABAergic compounds would generalise to it. MATERIALS AND METHODS: Rats were trained to discriminate tiagabine (30 mg/kg p.o.) from vehicle, and generalisation to drugs that modulate GABA was assessed. RESULTS: Gaboxadol (5-20 mg/kg p.o.), a selective extrasynaptic GABA A agonist, generalised to tiagabine, although the extent of the generalisation was inconclusive. Indiplon (1 mg/kg p.o.), a benzodiazepine-like hypnotic, also partially generalised to tiagabine, although zolpidem and S-zopiclone did not. Baclofen, a GABA B receptor agonist, and gabapentin, which increases synaptic GABA, did not generalise to tiagabine. (+)-Bicuculline (3 mg/kg i.p.), a GABA A receptor antagonist, blocked the tiagabine cue, but the less brain-penetrant salt form, bicuculline methochloride, had no effect. CONCLUSIONS: These data suggest that tiagabine generates a discriminative stimulus in rats, and provides a central GABA-mediated cue, but is distinct from the other GABAergic compounds tested.


Assuntos
Anticonvulsivantes/farmacologia , Aprendizagem por Discriminação/efeitos dos fármacos , GABAérgicos/farmacologia , Ácidos Nipecóticos/farmacologia , Administração Oral , Aminas/farmacologia , Animais , Compostos Azabicíclicos/farmacologia , Baclofeno/farmacologia , Benzodiazepinas/farmacologia , Bicuculina/análogos & derivados , Bicuculina/farmacologia , Encéfalo/efeitos dos fármacos , Ácidos Cicloexanocarboxílicos/farmacologia , Relação Dose-Resposta a Droga , Agonistas GABAérgicos/farmacologia , Antagonistas GABAérgicos/farmacologia , Proteínas da Membrana Plasmática de Transporte de GABA/efeitos dos fármacos , Gabapentina , Generalização do Estímulo/efeitos dos fármacos , Hipnóticos e Sedativos/farmacologia , Injeções Intraperitoneais , Isoxazóis/farmacologia , Masculino , Piperazinas/farmacologia , Piridinas/farmacologia , Ratos , Tiofenos/farmacologia , Tiagabina , Zolpidem , Ácido gama-Aminobutírico/farmacologia
2.
Neuropharmacology ; 52(3): 844-53, 2007 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-17196996

RESUMO

Gaboxadol is a selective extrasynaptic GABA(A) receptor agonist (SEGA) which enhances slow-wave sleep, and may act principally at extrasynaptic GABA(A)alpha4betadelta receptors. Drug discrimination is a very useful approach for exploring in vivo pharmacological similarities and differences between compounds and was therefore used to compare gaboxadol and zolpidem, an established hypnotic drug, against zopiclone, S-zopiclone, indiplon and tiagabine, all of which have been reported to enhance sleep. Gaboxadol generalised to itself, but not to zolpidem, zopiclone, S-zopiclone, R-zopiclone, indiplon or tiagabine. By contrast, zolpidem generalised to itself, zopiclone, S-zopiclone and indiplon, but not to R-zopiclone (the inactive enantiomer of zopiclone), gaboxadol or tiagabine. This suggests that zolpidem, zopiclone, S-zopiclone and indiplon share a discriminative stimulus, which may be mediated by their efficacy at GABA(A)alpha1betagamma receptors. Gaboxadol and tiagabine each have a different discriminative stimulus from all the other drugs tested.


Assuntos
Aprendizagem por Discriminação/efeitos dos fármacos , Agonistas GABAérgicos/farmacologia , Generalização Psicológica/efeitos dos fármacos , Isoxazóis/farmacologia , Sono/efeitos dos fármacos , Animais , Condicionamento Operante/efeitos dos fármacos , Relação Dose-Resposta a Droga , Avaliação de Medicamentos , Interações Medicamentosas , Masculino , Ratos , Ratos Sprague-Dawley
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